Target General Infomation
Target ID
T10052
Former ID
TTDR00786
Target Name
G1/S-specific cyclin E1
Gene Name
CCNE1
Synonyms
Cyclin E; G1/S-specific cyclin E; CCNE1
Target Type
Discontinued
Disease Retinoblastoma [ICD10: C69.2]
Function
Essential for the control of the cell cycle at the G1/S (start) transition.
Target Validation
T10052
UniProt ID
Sequence
MPRERRERDAKERDTMKEDGGAEFSARSRKRKANVTVFLQDPDEEMAKIDRTARDQCGSQ
PWDNNAVCADPCSLIPTPDKEDDDRVYPNSTCKPRIIAPSRGSPLPVLSWANREEVWKIM
LNKEKTYLRDQHFLEQHPLLQPKMRAILLDWLMEVCEVYKLHRETFYLAQDFFDRYMATQ
ENVVKTLLQLIGISSLFIAAKLEEIYPPKLHQFAYVTDGACSGDEILTMELMIMKALKWR
LSPLTIVSWLNVYMQVAYLNDLHEVLLPQYPQQIFIQIAELLDLCVLDVDCLEFPYGILA
ASALYHFSSSELMQKVSGYQWCDIENCVKWMVPFAMVIRETGSSKLKHFRGVADEDAHNI
QTHRDSLDLLDKARAKKAMLSEQNRASPLPSGLLTPPQSGKKQSSGPEMA
Drugs and Mode of Action
Drug(s) PD-0183812 Drug Info Terminated Retinoblastoma [547217]
Inhibitor (2'Z,3'E)-5-Chloro-5'-chloro-indirubin-3'-oxime Drug Info [530823]
(2'Z,3'E)-5-Chloro-5'-fluoro-indirubin-3'-oxime Drug Info [530823]
(2'Z,3'E)-5-Chloro-5'-hydroxy-indirubin-3'-oxime Drug Info [530823]
(2'Z,3'E)-5-Chloro-5'-methyl-indirubin-3'-oxime Drug Info [530823]
(2'Z,3'E)-5-Fluoro-5'-chloro-indirubin-3'-oxime Drug Info [530823]
(2'Z,3'E)-5-Fluoro-5'-fluoro-indirubin-3'-oxime Drug Info [530823]
(2'Z,3'E)-5-Fluoro-5'-hydroxy-indirubin-3'-oxime Drug Info [530823]
(2'Z,3'E)-5-Fluoro-5'-methoxy-indirubin-3'-oxime Drug Info [530823]
(2'Z,3'E)-5-Fluoro-5'-methyl-indirubin-3'-oxime Drug Info [530823]
(2'Z,3'E)-5-Nitro-5'-chloro-indirubin-3'-oxime Drug Info [530823]
(2'Z,3'E)-5-Nitro-5'-fluoro-indirubin-3'-oxime Drug Info [530823]
(2'Z,3'E)-5-Nitro-5'-hydroxy-indirubin-3'-oxime Drug Info [530823]
(2'Z,3'E)-5-Nitro-5'-methoxy-indirubin-3'-oxime Drug Info [530823]
(2'Z,3'E)-5-Nitro-5'-methyl-indirubin-3'-oxime Drug Info [530823]
2-((3,5-diamino-1H-pyrazol-4-yl)diazenyl)phenol Drug Info [528490]
3,4-di-(4-methoxyphenyl)-1H-pyrrole-2,5-dione Drug Info [528032]
3,4-diphenyl-1H-pyrrole-2,5-dione Drug Info [528032]
3-((3,5-diamino-1H-pyrazol-4-yl)diazenyl)phenol Drug Info [528490]
3-(4-methoxyphenyl)-4-phenyl-1H-pyrrole-2,5-dione Drug Info [528032]
3-(indole-3-yl)-4-phenyl-1H-pyrrole-2,5-dione Drug Info [528032]
4-(7-Butyl-5H-pyrrolo[2,3-b]pyrazin-6-yl)-phenol Drug Info [526504]
4-[(3,5-diamino-1H-pyrazol-4-yl)diazenyl]phenol Drug Info [528490]
5-nitroindirubin-3'-oxime Drug Info [530823]
BMS-536924 Drug Info [527711]
PD-0183812 Drug Info [525924]
Pathways
KEGG Pathway Cell cycle
Oocyte meiosis
p53 signaling pathway
PI3K-Akt signaling pathway
Hepatitis B
Measles
Pathways in cancer
Viral carcinogenesis
MicroRNAs in cancer
Prostate cancer
Small cell lung cancer
NetPath Pathway IL2 Signaling Pathway
TCR Signaling Pathway
PANTHER Pathway Cell cycle
Parkinson disease
p53 pathway
p53 pathway feedback loops 2
Pathway Interaction Database Signaling events mediated by PRL
E2F transcription factor network
mTOR signaling pathway
FOXM1 transcription factor network
BARD1 signaling events
PLK3 signaling events
Regulation of retinoblastoma protein
Reactome E2F mediated regulation of DNA replication
G0 and Early G1
SCF(Skp2)-mediated degradation of p27/p21
DNA Damage/Telomere Stress Induced Senescence
Cyclin E associated events during G1/S transition
G1/S-Specific Transcription
p53-Dependent G1 DNA Damage Response
WikiPathways DNA Damage Response
ID signaling pathway
G1 to S cell cycle control
Retinoblastoma (RB) in Cancer
Integrated Pancreatic Cancer Pathway
Parkinsons Disease Pathway
Parkin-Ubiquitin Proteasomal System pathway
Signaling Pathways in Glioblastoma
TSH signaling pathway
Mitotic G1-G1/S phases
Cell Cycle
miRNAs involved in DNA damage response
miRNA Regulation of DNA Damage Response
Androgen receptor signaling pathway
References
Ref 547217Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800014130)
Ref 525924J Med Chem. 2000 Nov 30;43(24):4606-16.Pyrido[2,3-d]pyrimidin-7-one inhibitors of cyclin-dependent kinases.
Ref 526504J Med Chem. 2003 Jan 16;46(2):222-36.Aloisines, a new family of CDK/GSK-3 inhibitors. SAR study, crystal structure in complex with CDK2, enzyme selectivity, and cellular effects.
Ref 527711J Med Chem. 2005 Sep 8;48(18):5639-43.Discovery of a (1H-benzoimidazol-2-yl)-1H-pyridin-2-one (BMS-536924) inhibitor of insulin-like growth factor I receptor kinase with in vivo antitumor activity.
Ref 528032J Med Chem. 2006 Feb 23;49(4):1271-81.Design, synthesis, and biological evaluation of 3,4-diarylmaleimides as angiogenesis inhibitors.
Ref 528490J Med Chem. 2006 Nov 2;49(22):6500-9.4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects.
Ref 530823J Med Chem. 2010 May 13;53(9):3696-706.5,5'-substituted indirubin-3'-oxime derivatives as potent cyclin-dependent kinase inhibitors with anticancer activity.
Ref 1587926URL: https://www.ebi.ac.uk/chembl/ The ChEMBL database in 2017

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